School Of Basic And Applied Sciences

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Author: search.filters.author.Jaitak, VikasHas files: Yes

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    Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies
    (Elsevier, 2020) Dhiman, N; Kaur, K; Jaitak, Vikas
    Cancer is a leading cause of death worldwide. Even after the availability of numerous drugs and treatments in the market, scientists and researchers are focusing on new therapies because of their resistance and toxicity issues. The newly synthesized drug candidates are able to demonstrate in vitro activity but are unable to reach clinical trials due to their rapid metabolism and low bioavailability. Therefore there is an imperative requisite to expand novel anticancer negotiators with tremendous activity as well as in vivo efficacy. Tetrazole is a promising pharmacophore which is metabolically more stable and acts as a bioisosteric analogue for many functional groups. Tetrazole fragment is often castoff with other pharmacophores in the expansion of novel anticancer drugs. This is the first systematic review that emphasizes on contemporary strategies used for the inclusion of tetrazole moiety, mechanistic targets along with comprehensive structural activity relationship studies to provide perspective into the rational design of high-efficiency tetrazole-based anticancer drug candidates. - 2020 Elsevier Ltd
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    Stevia rebaudiana targeting α-amylase: An in-vitro and in-silico mechanistic study
    (Taylor and Francis, 2019) Singla, R; Singla, N; Jaitak, Vikas
    Diabetes mellitus (DM) is the fastest growing metabolic disorder in the world. Recently, more attention is paid to the study of natural products due to side effects of synthetic drugs. Stevia rebaudiana (Bertoni) is considered an encouraging starting point for the antidiabetic lead development. In the present study, the in vitro α-amylase inhibitory activity of the extracts of S. rebaudiana is investigated. In order to understand the molecular mechanism and future pharmacophore development, in silico study of secondary metabolites isolated from S. rebaudiana was carried out. Results indicated that water extract shows highest α-amylase inhibitory activity as compared to other extracts. Moreover, compound 20 (rebaudioside A) which has been previously reported and isolated from water extract showed the impressive binding profile with α-amylase. Therefore, our study suggests that S. rebaudiana could be used in the development of therapeutic drugs for the treatment of diabetes. © 2017, © 2017 Informa UK Limited, trading as Taylor & Francis Group.
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    Natural products as multidrug resistance modulators in cancer
    (Elsevier, 2019) Kumar, Amit; Jaitak, Vikas
    Cancer is a prominent cause of death globally. Currently, many drugs that are in clinical practice are having a high prevalence of side effect and multidrug resistance. Risk of tumors acquiring resistance to chemotherapy (multidrug resistance) remains a significant hurdle to the successful treatment of various types of cancer. Membrane-embedded drug transporters, generally overexpressed in cancer, are the leading cause among multiple mechanisms of multidrug resistance (MDR). P-glycoprotein (P-gp) also MDR1/ABCB1, multidrug resistance associated protein 1 (MRP1/ABCC1), MRP2 and breast cancer resistance protein (BCRP/ABCG2) are considered to be a prime factor for induction of MDR. To date, several chemical substances have been tested in a number of clinical trials for their MDR modulatory activity which are not having devoid of any side effects that necessitates to find newer and safer way to tackle the current problem of multidrug resistance in cancer. The present study systematically discusses the various classes of natural products i.e flavonoids, alkaloids, terpenoids, coumarins (from plants, marine, and microorganisms) as potential MDR modulators and/or as a source of promising lead compounds. Recently a bisbenzyl isoquinoline alkaloid namely tetrandrine, isolated from Chinese herb Stephania tetrandra (Han-Fang-Chi) is in clinical trials for its MDR reversal activity. © 2019 Elsevier Masson SAS
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    Recent Advances in Plant Metabolites Analysis, Isolation, and Characterization
    (Springer, 2018) Singla, Ramit; Jaitak, Vikas
    Metabolites from natural sources either from terrestrial or marine sources serve as unmatched resources for new drug leads or diverse chemical identity. Due to ever-rising requirement for new pharmacophore in high-throughput screening and discovery for therapeutic drugs from metabolites, there has been motivated interest particularly in edible plants around the globe. Bioactive compounds are indispensable component present in different forms of botanicals, nutraceuticals, and herbal preparations used for the various medicinal applications. The prime focus in present chapter is to enlighten and discus diverse analytical methodologies which have been applied during extraction, isolation, and characterization of active constituents in botanicals, nutraceutical, and herbal preparations.
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    Identification of novel indole based heterocycles as selective estrogen receptor modulator.
    (Elsevier, 2018) Singla, Ramit; Prakash, Kunal; Gupta Kunj Bihari; Upadhyay, Shishir; Dhiman, Monisha; Jaitak, Vikas
    In the present study, we have designed and synthesized indole derivatives by coalescing the indole nucleus with chromene carbonitrile and dihydropyridine nucleus. Two compounds 5c and 6d were selected from series I and II after sequential combinatorial library generation, docking, absorption, distribution, metabolism and excretion (ADME) filtering, anti-proliferative activity, cytotoxicity, and ER-α competitor assay kit by utilizing estrogen receptor-α (ER-α) dominant T47D BC cells line and PBMCs (Peripheral Blood Mononuclear Cells). Cell imaging experiment suggested that both the compounds successfully cross cellular biomembrane and accumulate in nuclear, cytoplasmic and plasma membrane region. Semiquantitative RT-PCR and Western blotting experiments further supported that both compounds reduced the expression of mRNA and receptor protein of ER-α, thereby preventing downstream transactivation and signaling pathway in T47D cells line. Current findings imply that 5cand 6d represent novel ER-α antagonists and may be used in the development of chemotherapy for the management of BC.
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    Invitro anti-mutagenic potential of potentilla fulgens: A western himalayan plant
    (Informatics Publishing Limited, 2014) Monga, P.; Kaur, R.; Jaitak, Vikas
    Invitro anti-mutagenic potential of different extracts/fractions of Potentilla fulgens has been made by an Ames histidine reversion assay using TA98 and TA100 tester strains of Salmonella typhimurium against the direct-acting mutagens, 4-Nitro-O-phenylenediamine (NPD) and Sodium azide. P. fulgens has been used in traditional system of medicine as anti-hyperglycemic, hypoglycemic, anti-hyperlipidemic, anti-oxidant, anti-inflammatory and anti-ulcerogenic agent. Results indicated that n-butanol and water fractions showed strong inhibition activity against the mutagens (NPD, Sodium azide) in both co-incubation as well as pre-incubation treatments in TA98 and TA100 tester strains. ? 2017, Informatics Publishing Limited. All rights reserved.
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    Identification of novel indole based heterocycles as selective estrogen receptor modulator
    (Academic Press Inc., 2018) Singla, Ramit; Prakash, Kunal; Bihari Gupta, Kunj; Upadhyay, Shishir; Dhiman, Monisha; Jaitak, Vikas
    In the present study, we have designed and synthesized indole derivatives by coalescing the indole nucleus with chromene carbonitrile and dihydropyridine nucleus. Two compounds 5c and 6d were selected from series I and II after sequential combinatorial library generation, docking, absorption, distribution, metabolism and excretion (ADME) filtering, anti-proliferative activity, cytotoxicity, and ER-? competitor assay kit by utilizing estrogen receptor-? (ER-?) dominant T47D BC cells line and PBMCs (Peripheral Blood Mononuclear Cells). Cell imaging experiment suggested that both the compounds successfully cross cellular biomembrane and accumulate in nuclear, cytoplasmic and plasma membrane region. Semiquantitative RT-PCR and Western blotting experiments further supported that both compounds reduced the expression of mRNA and receptor protein of ER-? thereby preventing downstream transactivation and signaling pathway in T47D cells line. Current findings imply that 5c and 6d represent novel ER-? antagonists and may be used in the development of chemotherapy for the management of BC. ? 2018 Elsevier Inc.
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    Essential Oils: New Perspectives in Human Health and Wellness.
    (Hindawi, 2014) Firenzuoli, Fabio; Jaitak, Vikas; Horvath, Gyorgyi; Bassole, Imael Henri Nestor; Setzer,William N.; Gori, Luigi
    Essential oils are natural products, derived from aromatic plants, traditionally used all over the world for disinfection, as anti-inflammatory, relaxing, and stimulating substances, and with potential and modern exploitation in clinical medicine. The earliest recorded mention of the techniques and methods used to produce essential oils is believed to be that of Ibn al-Baitar (1188�1248). The chemical composition of these essential oils varies widely depending upon the geographical location, botanical origin, genetics, bacterial endophytes, and extraction techniques. Essential oils are commonly used in food and cosmetic industries. They can be used as natural alternatives to synthetic preparations to prevent and treat infectious diseases. They are used traditionally to treat other diseases like respiratory tract, digestive system, gynecological, andrological, endocrine, cardiovascular, nervous system, and skin infections. Many of them have shown anticancer activities, too.
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    Polymeric Encapsulates of Essential Oils and Their Constituents: A Review of Preparation Techniques, Characterization, and Sustainable Release Mechanisms
    (Taylor and Francis Inc., 2016) Vishwakarma, G.S.; Gautam, N.; Babu, J.N.; Mittal, S.; Jaitak, Vikas
    Natural polymer based encapsulation of essential oil (EO) is one of the emerging and challenging area of research in perfumery, cosmetics, flavoring agents, preservatives, therapeutics, etc. The knowledge of formulation techniques and physico-chemical properties of the polymers are the basic requirements for the successful encapsulations of essential oils (EOs). This current review article is focused on a comparative account of various formulation techniques based on their applicability. For the first time, it also reviews various physico-chemical techniques used in the analysis of EO encapsulates to determine their stability, structure, surface morphology, and encapsulation efficiency. Further, the mechanisms involved in the release of EOs from encapsulates, along with various factors affecting their release, have also been discussed. ? 2016 Taylor & Francis Group, LLC.
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    Antimicrobial and repellent activity of the essential oils of two lamiaceae cultivated in Western Himalaya
    (Bentham Science Publishers B.V., 2015) Stappen, Iris; Ali, Abbas; Tabanca, Nurhayat; Khan,Ikhlas A.; Wanner, J�rgen; Gochev, Velizar K.; Singh, Virendra; Lal, Brij; Jaitak, Vikas; Kaul, Vijay K.; Schmidt, Erich; Jirovetz, Leopold; Stappen, I.; Ali, A.; Tabanca, N.; Khan, I.A.; Wanner, J.; Gochev, V.K.; Singh, V.; Lal, B.; Jaitak, V.; Kaulh, V.K.; Schmidt, E.; Jirovetz, L.
    The essential oils of two Lamiaceae cultivated in Western Himalaya were examined on their antimicrobial, biting deterrent as well as larvicidal activity. Additionally their odors are described and their chemical compositions analyzed by GC-MS are given. The main component of Nepeta cataria oil was 4a?,7?,7a?-nepetalactone (85%), whereas camphor (27%) and 1,8-cineol (27%) were dominant in the oil of Rosmarinus officinalis. The studied essential oils demonstrated high to moderately antimicrobial activity against reference strains, clinical and food spoilage isolates of Bacillus cereus, Staphylococcus aureus, Escherichia coli, Salmonella abony and Candida albicans (MIC 160-640 ?g/ml) and indicated low activity against Pseudomonas aeruginosa and P. fluorescens. Both oils showed biting deterrent activity above solvent control but lower than DEET. Nepeta catarica essential oil exhibited high toxicity with LD50 value of 20.2 whereas R. officinalis oil showed only 50% mortality at the highest tested dose of 125 ppm against 1-day old Aedes aegypti larvae at 24-hour post treatment. ? 2015 Bentham Science Publishers.